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BGJ398 (NVP-BGJ398)

NVP-BGJ398 (200x200px)
  • NVP-BGJ398 (200x200px)
  • NVP-BGJ398 (600x600px)
Price:
$109.00
Catalog #:
C6245-5
Quantity:

Product Description

NVP-BGJ398 (BGJ398), discovered in 2011, is a potent pan inhibitor of the fibroblast growth factor receptor (FGF) tyrosine kinases. BGJ398 inhibits FGFR1, FGFR2, and FGFR3 with IC50 values of 0.9 nM, 1.4 nM, and 1 nM respectively in in vitro evaluation. [1] BGJ398 also inhibits FGFR4, VEGFR2, Abl, Fyn, Kit, Lck, Lyn and Yes, with significantly lower potencies. In an in vivo test, BGJ398 showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3. [1]
BGJ398 is currently being tested in a Phase II clinical trial in advanced cholangiocarcinoma (CCA) patients with FGFR genetic alterations for anti-tumor activity and safety profile. [2] [3]

Technical information:

Chemical Formula:   C26H31Cl2N7O3
CAS #:   872511-34-7
Molecular Weight:   560.48
Purity:   > 98%
Appearance:   white
Chemical Name:   3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea
Solubility:   Up to 1 mM in DMSO
Synonyms:   BGJ398, NVP-BGJ398

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.

Reference:

1. Guagnano V, et al. Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011; 54(20):7066-83 Pubmed ID: 21936542
2. A Phase II, Single Arm Study of BGJ398 in Patients With Advanced Cholangiocarcinoma.  clinicaltrials.gov/NCT02150967 
3. Milind M. Javle, et al. A phase 2 study of BGJ398 in patients (pts) with advanced or metastatic FGFR-altered cholangiocarcinoma (CCA) who failed or are intolerant to platinum-based chemotherapy. J Clin Oncol. 2016; 34(4) suppl:335

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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